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ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM. ACY-738 has a selectivity of 60- to 1500-fold over class I HDACs. ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells[1]. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228.
In vivo, ACY-738 induces dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors in novel, but not familiar environments. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels.
| Molecular Weight | 270.29 |
| Formula | C14H14N4O2 |
| CAS Number | 1375465-91-0 |
| Solubility (25°C) | DMSO: ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
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| Belinostat
Belinostat (PXD101) is a novel HDAC inhibitor with an IC50 of 27 nM. |
| CUDC-101
CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. |
| Givinostat hydrochloride monohydrate
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor. The IC50 values for maize HDAC preparations HD2, HD-1B and HD-1A are 10, 7.5 and 16 nM respectively. |
| Niltubacin
Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. |
| Tubacin
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. |
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